104 results about "Gemcitabine Hydrochloride" patented technology

A process for preparation of gemcitabine hydrochloride and purification thereof.

The invention discloses a gemcitabine hydrochloride liposome injection and a preparation method thereof. The gemcitabine hydrochloride liposome injection is prepared from the following components in specific percentage by weight: gemcitabine hydrochloride, cholesterol, egg yolk phosphatidylinositol, phosphatidylcholine, tween 80, trehalose, mannitol and polyvinylpyrrolidone. The liposome injection is high in stability and cannot be cracked due to fusion, ice crystal and the like during freezing; and after long-term storage, liposome is still high in package rate. According to the gemcitabine hydrochloride liposome injection, the solubility of gemcitabine hydrochloride is improved; the quality of a product is improved; the toxic and side effects are reduced; the retention time of medicines during general circulation is prolonged; the biological utilization rate of the medicine is increased; the treating effect is obviously enhanced; the preparation method is simple; and the gemcitabine hydrochloride liposome injection is suitable for industrial large-scale production.

The invention discloses a method for synthesizing an important intermediate 2-deoxy-2, 2-difluorofuran ribose compound of gemcitabine hydrochloride and a method for synthesizing the gemcitabine hydrochloride by using the compound as a raw material under the catalysis of cytosine. The method has good stereo selectivity, a mild reaction condition, easily obtained raw materials, low pollution and high yield, and is suitable for industrialized production.

The invention belongs to the field of pharmacy, which discloses hydrochloric gemcitabine or gemcitabine composition. The composition comprises components in the following weight ratio: the ratio of hydrochloric gemcitabine or gemcitabine, polymer and protein is 0.1 to 20:0.00 to 50:0.00 to 20, wherein, the weight of polymer and protein is not zero at the same time. The composition can effectively prevent hydrochloric gemcitabine or gemcitabine from loosing the activity in vivo, and has the advantages of good stability, low toxicity and good efficacy.

The invention relates to a 2-deoxidized-2, 2-hydrochloric acid difluoro deoxycytidine compound as shown in a formula (I), and discloses a method for preparing gemcitabine hydrochloride. The method is simple in process, high in yield and quite suitable for industrial production, the purity of a product is fine, and harsh reaction conditions are omitted.

The invention relates to a gemcitabine hydrochloride purifying method. The gemcitabine hydrochloride purifying method comprises the following steps: a), dissolving a gemcitabine hydrochloride coarse product into water, regulating the pH of the solution to 8-9 by adding alkali, stirring and reacting, and extracting to obtain gemcitabine; b), dissolving the gemcitabine into an alcohol solution, with the concentration of 0.1-0.2g / mL, adding activated carbon, filtering, and collecting filtrate; c), separating the filtrate with a preparing chromatographic column, wherein a fluid phase used by the chromatographic column is acetone or acetonitrile and a hydrochloric acid solution, the volume ratio of acetone or acetonitrile to the hydrochloric acid solution is 30-50: 70-50, and a stationary phase filler is silica or aluminum oxide; collecting filtrate; and drying to obtain a gemcitabine hydrochloride refined product. Through acid-base reaction, activated carbon adsorption, and separation and purification of the preparing chromatographic column, the purity of the gemcitabine hydrochloride is improved, the quality of a prepared product is optimized and the safety of clinical medicine is ensured; and the method is simple in process and low in cost and is applicable to industrial production.

The invention relates to a gemcitabine hydrochloride lyophilized composition and a preparation method thereof, and aims to solve the technical problems of poor stability and long production cycle in the current gemcitabine hydrochloride lyophilized preparation. The gemcitabine hydrochloride lyophilized composition comprises the following components: gemcitabine hydrochloride, cyclodextrin or cyclodextrin derivative, lyophilized excipient and pH regulator, wherein the weight proportion of the components is 1:0.2-0.55:0.2-0.7:0.01-0.1. The gemcitabine hydrochloride lyophilized composition and the preparation method thereof have the benefits that a proper amount of solubilizer (cyclodextrin or cyclodextrin derivative) is added to the gemcitabine hydrochloride lyophilized composition, so thatthe solubility of gemcitabine hydrochloride can be enhanced, the preparation has good reconfigurability and stability, the production cycle of medicine is shortened, the energy consumption is reduced, the gemcitabine hydrochloride lyophilized composition is convenient to store and transport, and security is provided for clinical medication.

The present invention discloses a gemcitabine hydrochloride lyophilized preparation. The lyophilized preparation comprises, by weight, 20-70 parts of gemcitabine hydrochloride, 15-60 parts of a lyoprotectant and 0.005-0.5 parts of an antioxidant. Compared to the prior art, with the gemcitabine hydrochloride lyophilized preparation provided by the present invention, the problem of the stability ofthe gemcitabine hydrochloride is solved; the product quality is ensured; the risk of drug using is reduced; the preparation process is simple, the cost is low; and the preparation is suitable for theindustrial production, and has practical value.

The invention relates to a compound in a formula (I), and discloses a method for preparing gemcitabine hydrochloride. The method includes preparing an intermediate type (III) compound by means of realizing Reformatsky reaction, removing a protecting group and realizing lactonization and double benzoylation; obtaining a compound in a formula (VI) via reduction, methyl sulfonylation and condensation; and finally removing a protecting group, saltifying and realizing crystallization to obtain a final product. The method is simple in process, high in yield and quite suitable for industrial production, the purity of the product is fine, and harsh reaction conditions are omitted.

The invention discloses a gemcitabine hydrochloride liposome injection and a preparation method thereof. The gemcitabine hydrochloride liposome injection is prepared from the following components in specific percentage by weight: gemcitabine hydrochloride, cholesterol, egg yolk phosphatidylinositol, phosphatidylcholine, tween 80, trehalose, mannitol and polyvinylpyrrolidone. The liposome injection is high in stability and cannot be cracked due to fusion, ice crystal and the like during freezing; and after long-term storage, liposome is still high in package rate. According to the gemcitabine hydrochloride liposome injection, the solubility of gemcitabine hydrochloride is improved; the quality of a product is improved; the toxic and side effects are reduced; the retention time of medicines during general circulation is prolonged; the biological utilization rate of the medicine is increased; the treating effect is obviously enhanced; the preparation method is simple; and the gemcitabine hydrochloride liposome injection is suitable for industrial large-scale production.